title: In vitro and in vivo anticancer activity of extracts, fractions, and eupomatenoid-5 obtained from Piper regnellii leaves.
abstract: Despite numerous studies with the Piper genus, there are no previous results reporting in vitro or in vivo Piper regnellii (Miq.) C. DC. var. regnellii anticancer activity. The aim of this study was to investigate P. regnellii in vitro and in vivo anticancer activity and further identify its active compounds. In vitro antiproliferative activity was evaluated in 8 human cancer cell lines: melanoma (UACC-62), breast (MCF7), kidney (786-0), lung (NCI-H460), prostate (PC-3), ovary (OVCAR-3), colon (HT29), and leukemia (K-562). Total growth inhibition (TGI) values were chosen to measure antiproliferative activity. Among the cell lines evaluated, eupomatenoid-5 demonstrated better in vitro antiproliferative activity towards prostate, ovary, kidney, and breast cancer cell lines. In vivo studies were carried out with Ehrlich solid tumor on Balb/C mice treated with 100, 300, and 1000 mg/kg of P. regnellii leaves dichloromethane crude extract (DCE), with 30 and 100 mg/kg of the active fraction (FRB), and with 30 mg/kg of eupomatenoid-5. The i. p. administration of DCE, FRB, and eupomatenoid-5 significantly inhibited tumor progression in comparison to control mice (saline). Therefore, this study showed that neolignans of Piper regnellii have promising anticancer activity. Further studies will be undertaken to determine the mechanism of action and toxicity of these compounds.
authors.affiliation: Programa de Pós-graduação em Biologia Celular e Estrutural, Instituto de Biologia, Universidade Estadual de Campinas - UNICAMP, Campinas, SP, Brasil.
authors.forename: Giovanna Barbarini
authors.initials: GB
authors.lastname: Longato
authors.forename: Larissa Yokota
authors.initials: LY
authors.lastname: Rizzo
authors.forename: Ilza Maria de Oliveira
authors.initials: IM
authors.lastname: Sousa
authors.forename: Sirlene Valério
authors.initials: SV
authors.lastname: Tinti
authors.forename: Ana
authors.initials: A
authors.lastname: Possenti
authors.forename: Glyn Mara
authors.initials: GM
authors.lastname: Figueira
authors.forename: Ana Lúcia Tasca Gois
authors.initials: AL
authors.lastname: Ruiz
authors.forename: Mary Ann
authors.initials: MA
authors.lastname: Foglio
authors.forename: João Ernesto
authors.initials: JE
authors.lastname: de Carvalho
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001572:Benzofurans / Q000737:chemistry / Q000494:pharmacology*; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy; D045744:Cell Line, Tumor; D005260:Female; D006801:Humans; D017705:Lignans / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D010636:Phenols / Q000737:chemistry / Q000494:pharmacology*; D031701:Piper / Q000737:chemistry*; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D018515:Plant Leaves / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D001572:Benzofurans; D017705:Lignans; D010636:Phenols; D010936:Plant Extracts; C452811:eupomatenoid 5